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PHA-665752 C-Met inhibitor,potent and ATP-competitive

Catalog No.A2307
Size Price Stock Qty
10mM (in 1mL DMSO)
$90.00
In stock
Evaluation Sample
$28.00
In stock
10mg
$80.00
In stock
50mg
$330.00
In stock
100mg
$570.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

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Sample solution is provided at 25 µL, 10mM.

Product Citations

1. Xia Y, Xia YF, et al. "Madecassoside ameliorates bleomycin-induced pulmonary fibrosis in mice through promoting the generation of hepatocyte growth factor via PPAR-γ in colon. Br J Pharmacol." 2016 Apr;173(7):1219-35.  PMID:26750154

Quality Control

Quality Control & MSDS

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Chemical structure

PHA-665752

Related Biological Data

PHA-665752

Related Biological Data

PHA-665752

Related Biological Data

PHA-665752

Biological Activity

Description PHA-665752 is a potent, selective and ATP-competitive inhibitor of c-Met with IC50 of 9 nM, >50-fold selectivity for c-Met than RTKs or STKs.
Targets c-Met          
IC50 9 nM          

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Chemical Properties

Cas No. 477575-56-7 SDF Download SDF
Chemical Name (3Z)-5-[(2,6-dichlorophenyl)methylsulfonyl]-3-[[3,5-dimethyl-4-[(2R)-2-(pyrrolidin-1-ylmethyl)pyrrolidine-1-carbonyl]-1H-pyrrol-2-yl]methylidene]-1H-indol-2-one
Canonical SMILES CC1=C(NC(=C1C(=O)N2CCCC2CN3CCCC3)C)C=C4C5=C(C=CC(=C5)S(=O)(=O)CC6=C(C=CC=C6Cl)Cl)NC4=O
Formula C32H34Cl2N4O4S M.Wt 641.61
Solubility >32.1mg/mL in DMSO Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Research Update

1. Celastrol exerts synergistic effects with PHA-665752 and inhibits tumor growth of c-Met-deficient hepatocellular carcinoma in vivo. Mol Biol Rep. 2013 Jul;40(7):4203-9. doi: 10.1007/s11033-013-2501-y. Epub 2013 May 7.
Abstract
PHA665752 is a c-Met inhibitor that exhibits anti-tumor activity only in c-Met-positive tumor cells. The combination of PHA6657552 and Celastrol is a potential therapy of c-Met-deficient tumors for their demonstrated antitumor effects in c-Met-deficient hepatocellular carcinoma cells and xenografts.
2. A selective small molecule inhibitor of c-Met, PHA-665752, reverses lung premalignancy induced by mutant K-ras. Mol Cancer Ther. 2008 Apr;7(4):952-60. doi: 10.1158/1535-7163.MCT-07-2045.
Abstract
PHA-665752, a c-Met inhibitor, inhibited lung tumorigenesis in Kras(LA1) mice and induced apoptosis in LKR-13 cells and MECs, where apoptosis in MECs was induced by c-Met inhibition.
3. Amplification of MET may identify a subset of cancers with extreme sensitivity to the selective tyrosine kinase inhibitor PHA-665752. Proc Natl Acad Sci U S A. 2006 Feb 14;103(7):2316-21. Epub 2006 Feb 6.
Abstract
Gastric cancer cells with high levels of MET are extraordinarily susceptible to PHA-665752, which induces massive apoptosis.

Background

PHA-665752 is a potent, ATP-competitive and specific c-Met receptor tyrosine kinase inhibitor with K(i) value of 4 nM and IC50 value of 9nM. PHA-665752 shows more than 50-fold selectivity for c-Met versus other serine-threonine and tyrosine kinases [1].

PHA-665752 has been demonstrated to inhibit hepatocyte growth factor (HGF) and c-Met-mediated cell proliferation, motility, invasion and morphology of pancreatic carcinoma cells BxPC-3, gastric carcinoma cells GTL-16 and lung cancer cells NCI-H441. Additionally, PHA-665752 inhibits the c-MET downstream mediators phosphorylation induced by HGF [1].

In vivo, PHA-665752 inhibits c-Met phosphorylation as well as tumor growth in both S114 and GTL-16 implanted xenograft athymic mice [1].

References:
[1] Christensen JG1, Schreck R, Burrows J, Kuruganti P, Chan E, Le P, Chen J, Wang X, Ruslim L, Blake R, Lipson KE, Ramphal J, Do S, Cui JJ,Cherrington JM, Mendel DB. A selective small molecule inhibitor of c-Met kinase inhibits c-Met-dependent phenotypes in vitro and exhibits cytoreductive antitumor activity in vivo. Cancer Res. 2003 Nov 1;63(21):7345-55.